产品
编 号：F742792
分子式：C23H18F4N2O
分子量：414.4
分子式：C23H18F4N2O
分子量：414.4
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CAS No: 1159996-43-6
产品详情
生物活性：
AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM.
体内研究：
AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (Tb) in rats.Animal Model:Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age)
Dosage:30 mg/kg
Administration:Oral administration, once
Result:Produced a significant decrease of Tb from 40 min to 70 min post dosing.Effect of AMG8788 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCTCompoundDose mg/kg (route) Max Tb decrease (°C) P value * Time post dosing (min) Plasma concentration
AMG878830 (p.o.)0.53p < 0.05401.5 ± 0.6
体外研究：
AMG8788 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 6.7 h.
AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM.
体内研究：
AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (Tb) in rats.Animal Model:Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age)
Dosage:30 mg/kg
Administration:Oral administration, once
Result:Produced a significant decrease of Tb from 40 min to 70 min post dosing.Effect of AMG8788 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCTCompoundDose mg/kg (route) Max Tb decrease (°C) P value * Time post dosing (min) Plasma concentration
AMG878830 (p.o.)0.53p < 0.05401.5 ± 0.6
体外研究：
AMG8788 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 6.7 h.
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